200214-49-9

Upstream product

• 200214-48-8 tert-butyl N-[4-chloro-3-(hydroxymethyl)phenyl]carbamate 
• 124-63-0 methanesulfonyl chloride 
• 89951-56-4 4-chloro-5-hydroxymethyl aniline 
• 80866-80-4 2-chloro-5-nitrobenzyl alcohol 

Downstream Products

• 200214-50-2 (2-chloro-5-(Boc-amino)phenyl)acetonitrile 
• 934477-05-1 C₂₂H₃₀ClN₃O₇S 
• 934477-04-0 2-(5-tert-butoxycarbonylamino-2-chloro-phenyl)-acrylic acid ethyl ester 
• 200214-52-4 ethyl (2-chloro-5-(Boc-amino)phenyl)acetate 
• 409082-02-6 ethyl 2-(5-amino-2-chlorophenyl)acetate 

Relevant academic research and scientific papers

3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)

A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B. (-)2a displays TAFIa IC50 = 3 nM and 600-fold selectivity against CPN. Inhibition of TAFIa with (rac)2a resulted in dose dependent acceleration of human plasma clot lysis in vitro and was efficacious as an adjunct to tPA in an in vivo rabbit jugular vein thrombolysis model.

AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS

There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.